Ellipticine (Elliptisine) is a potent antineoplastic agent exhibiting multiple mechanisms of action, IC50 of 0.67±0.06, 1.25±0.13, 1.25±0.13, 0.67±0.06, 0.27±0.02, 0.49±0.04, 0.44±0.03, and 1.48±0.62 μM for Leukemia HL-60, Breast adenocarcinoma MCF-7, Breast adenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32, Neuroblastoma UKF-NB-4, Neuroblastoma UKF-NB-3, and Glioblastoma U87 mg cell, respectively.

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

Vinaxanthone (SM-345431) is a small molecule compound derived from Penicillium chrysogenum that is a selective and potent semaphorin3A, phospholipase C (PLC), and FabI inhibitor, inhibiting semaphorin3A and FabI.Vinaxanthone exhibits antimicrobial activity, blocking intracellular fatty acid synthesis and inhibiting the growth of Staphylococcus aureus.

DB21, Galectin-1 Antagonist, is a peptidomimetic conjugated with dibenzofuran, serving as an allosteric inhibitor of galectin-1 (GAL1) interactions with glycans on cell surfaces. This compound enhances the inhibition of angiogenesis and tumor growth in melanoma, lung adenocarcinoma, and ovarian cancer models [1].

Flemiphilippin A has antioxidant activity, it shows DPPH radical scavenging activity with effective half maximal concentration (EC50) of 18.36 ug/mL. Flemiphilippinin A (5 ug/mL) exhibits some level of antitumor activity against human hepatocellular carci

Pixinol, a natural glycoside, demonstrates cytotoxic effects on human lung carcinoma GLC4 and adenocarcinoma COLO 320 cell lines with IC50 values of 71 µM and 43 µM, respectively [1].

1-Decarboxy-3-oxo-ceanothic acid shows in vitro cytotoxic activity in a human ovarian adenocarcinoma cell line, the cytotoxic effect is mediated, at least in part, by the induction of apoptosis. It shows cytotoxic against OVCAR-3 and HeLa cancer cell line

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity[1][2]. DS-7423 increases TP53 expression, the level of p-TP53 on Ser-46, and induced apoptosisrelated TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1].DS-7423 also inhibits other isoforms of class I PI3K (IC50 values: PI3Kβ = 1,143 nM; PI3Kγ = 249 nM; PI3Kδ = 262 nM)[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62.[2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

Sartorypyrone B, a 2β-acetoxyl analogue of chevalone C, is derived from the ethyl acetate extract of the culture of Neosartorya tsunodae (KUFC 9213), a fungus associated with marine sponges. This compound demonstrates potent growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cancer cell lines with GI50 values of 17.8, 20.5, and 25.0 μM, respectively, indicating its potential in the study of breast adenocarcinoma, non-small cell lung cancer, and melanoma [1].

2β,3β,23α-Trihydroxy-12-oleanen-28-oic acid shows cytotoxic activities to human lung adenocarcinoma(A-549)cell lines. 2α,3β,23-Trihydroxyolean-12-en-28-oic acid and 2α,3β,23-trihydroxyurs-12-en-28-oic acid exhibit cytotoxicity in vitro against the growth of human cancer cells lines HepG-2,with IC50 values of 16.13 ± 3.83, 15.97 ± 2.47 uM, respectively.

1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone has moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, but lacks antifungal activity against Candida albicans.

Jatamanvaltrate B shows cytotoxicity against lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8),and hepatoma (Bel7402) cell lines.

Atalantoflavone shows urease inhibitory potential. It displays weak cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3.

Nidanilimab (CAN04) is a fully humanized IL1RAP monoclonal antibody with a Kd value of 1.10 pM. Nidanilimab has antitumor activity, cutting off the IL1α and IL1β signaling pathways and inducing the immune system to destroy tumor cells. Nidanilimab can be used to study solid cancers such as non-small cell lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC).

Xanthoxyletin shows potent antibacterial, fungicidal, and algicidal properties, it also has anticancer, and anti-inflammatory activities. It shows an inhibitory effect on iNOS protein expression at 10 microM, it also can inhibit the synthesis of nitric oxide and the protein expression of tumor necrosis factor-alpha and cyclooxygenase-2. Xanthoxyletin induces S phase arrest and apoptosis in human gastric adenocarcinoma SGC-7901 cells, the effects are associated with the DNA damage, apoptosis through mitochondrial dysfunction, and cell cycle arrest at S phase in a dose-dependent manner, it also can increase the production of reactive oxygen species.

Gresonitamab (AMG 910), a half-life extended (HLE) bispecific T-cell engager (BiTE) antibody, specifically targets CD3-positive T cells and CLDN18.2-expressing tumor cells, offering potential research applications in adenocarcinoma [1].

Dihydrodaidzin shows cytotoxic activities against human stomach carcinoma (Hs 740.T, Hs 756 T), breast adenocarcinoma (Hs 578 T, Hs 742.T), and prostate carcinoma (DU 145, LNCaP-FGC) cell lines.

5-Hydroxyuridine (OHUrd) is a purine nucleoside analogue with potential antitumour activity, showing cytotoxicity against human colon adenocarcinoma cell lines.

Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human adenocarcinoma cells. Moreover, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].

6-Prenylapigenin(4',5,7-Trihydroxy-6-prenylflavone) shows potent inhibitory activity on melanin formation, it may be potential sources for skin whitening agents. It also shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarci

P-gp/BCRP-IN-2 (compound 15), an oxadiazole derivative, functions as a dual inhibitor targeting both the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). Additionally, it bolsters the anti-proliferative impact of Doxorubicin in the drug-resistant HT29/DX and MDCK-MDR1 human adenocarcinoma colon cancer cell lines [1].

IST-622 is a unique topoisomerase inhibitor, showing significant growth-inhibitory effects against large-cell lung cancer (Lu-116) and gastric adenocarcinoma (St-4).

Antitumor agent-75 is a novel and potent antitumor agent. antitumor agent-75 has cytotoxic effects on cancer and normal human cell lines. antitumor agent-75 in combination with antitumor agent-74 exhibits a highly selective cytotoxic effect (IC50: 2.8 μM) against human lung adenocarcinoma (cell line A549). Antitumor agent-75 can be used in cancer research.

Retifanlimab, an anti-programmed cell death protein 1 (anti-PD-1) monoclonal antibody (mAb), is utilized in the research of gastroesophageal adenocarcinoma (GEA) [1].

Chrysomycin B is an antibiotic isolated from Streptomyces sp. Chrysomycin B induces DNA damage and inhibits topoisomerase II in the human lung adenocarcinoma A549 cell line.

1,4,5,6-Tetrahydroxy-7-prenylxanthone has anti-cancer activity, it shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines; it also exhibits moderate activities with GI50 (Growth inhibitory) values of 2.

Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 μM) in Cancer Cells.Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.antitumour

Chlorovaltrate K shows moderate cytotoxicity against lung adenocarcinoma (A 549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8) and hepatoma (Bel 7402) cell lines with IC50 values of 0.89-9.76 uM.

3-Hydroxybakuchiol exerts cytotoxic and anti-proliferative effects on the TA3/Ha mouse mammary adenocarcinoma cell line and induces a decrease in the mitochondrial transmembrane potential, the activation of caspase-3, the opening of the mitochondrial perm

Bostrycin, an anthraquinone derived from B. alpestre, exhibits a broad spectrum of biological activities including antibacterial, antiproliferative, and phytotoxic effects. This compound demonstrates efficacy against Gram-positive bacteria like methicillin-resistant S. aureus (MRSA), M. tuberculosis, and C. botulinum. Additionally, Bostrycin shows antiproliferative action against A549 lung adenocarcinoma cells, particularly by arresting the cell cycle at the G0/G1 phase and triggering apoptosis within a concentration range of 10 to 30 µM. As a phytotoxin, it causes necrosis in water hyacinth leaves at approximately 7 µg/ml. Furthermore, Bostrycin serves as a protein immobilization cross-linking agent, managing to preserve its bacteriostatic properties when affixed to nonwoven polypropylene fabric.

Eriocalyxin B induces apoptosis and cell cycle arrest in pancreatic adenocarcinoma cells through caspase- and p53-dependent pathways, should be considered a candidate for pancreatic cancer treatment; it is a specific inhibitor of STAT3, it directly target

BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0/G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg/kg) reduces tumor growth in an SW1990 mouse xenograft model. |1. Zhang, P., Li, X.-M., Wang, J.-N., et al. New butenolide derivatives from the marine-derived fungus Paecilomyces variotii with DPPH radical scavenging activity. Phytochem. Lett. 11, 85-88 (2015).|2. Sun, W., Luan, S., Qi, C., et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun. Signal. 17(1), 111 (2019).

Jolkinol A can inhibit both MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) cell lines, with GI50 values ranging between 40.9 microM and 95.3 microM.

Volvaltrate B shows cytotoxic activity against the lung adenocarcinoma (A549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8), and hepatoma (Bel7402) cell lines, with IC50 values of 8.5, 2.0, 3.2, and 6.1 uM, respectively.

10-Deacetylcephalomannin exhibits activity against PS leukemia in vivo; however, its instability leads to an equilibrium mixture with its cytotoxic C-7 epimer. Additionally, 10-Deacetylcephalomannine demonstrates growth inhibitory effects on human cancer cell lines, including cervical HeLa adenocarcinoma.

LY303511, a structural analog of LY294002, selectively inhibits mTOR-dependent phosphorylation of S6K, unlike its counterpart, which acts as a phosphatidylinositol 3-kinase (PI3K) inhibitor. It effectively reduces cell proliferation in human lung epithelial adenocarcinoma cells by hindering G2/M phase progression and suppressing casein kinase 2 activity. Additionally, LY303511 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitivity in HeLa cells resistant to TRAIL-induced apoptosis and blocks voltage-gated potassium (Kv) channels.

Oxythiamine chloride HCl is a thiamine antimetabolite that has anticancer activities. It is converted by thiamine pyrophosphokinase to oxythiamine pyrophosphate, a transketolase inhibitor. Oxythiamine decreases transketolase activity in breast cancer. It inhibits the nonoxidative synthesis of ribose and decreases RNA and DNA synthesis in pancreatic cancer. In vivo, oxythiamine induces cell cycle arrest at the G1 phase and apoptosis in an adenocarcinoma model. Oxythiamine, in combination with sorafenib, reduces tumor growth in an SMMC mouse xenograft model and has also been used to induce thiamine deficiency in mice.

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

Conicasterol displays marked cytotoxic activity against human breast adenocarcinoma cell line (MCF-7) with the IC50 value of 6.23 ug/mL.

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

3PO is a small-molecule inhibitor of PFKFB3 (IC50: 22.9 μM), inhibiting the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50: 1.4-24 μM). It suppresses glucose uptake, and decreases the intracellular concentration

Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor. Deltarasin can inhibit KRAS-PDEδ interactions by binding to a hydrophobic pocket on PDEδ, resulting in the impairment of cell growth, KRAS activity, and RAS/RAF signaling in human pancreatic ductal adenocarcinoma cell lines. The anti-cancer cell activity of deltarasin can be enhanced by simultaneously blocking tumor protective autophagy