l1210

5-fluorouridine is also known as FUrd, 5-Fluorouracil 1-beta-D-ribofuranoside, 5-Fur, or 5-Fluoro-uridine. 5-fluorouridine is a solid. This compound belongs to the pyrimidine nucleosides and analogues. These are compounds comprising a pyrimidine base attached to a sugar. 5-fluorouridine is known to target uridine phosphorylase. FUrd is often used in chemical and biochemical comparison studies with fluorouracil and thymine analogs.

Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.

4-Carboxyquinoline (4-Quinolinecarboxylic acid) showed anti-tumor activity against L1210 leukemia and B16 melanoma.

Podophyllotoxinone, a natural compound found in Dysosma versipellis, shows inhibitory activity against L1210 leukemia and KB cells in vitro.

1. 7-Ethylcamptothecin has the superior antitumor activity than CPT. (a). 7-Ethylcamptothecin has a stronger growth-inhibiting activity against tumor cells. (b). 7-Ethylcamptothecin remains in the intestinal tract for a longer time and in higher amounts when administered in vivo.

Cytarabine 5′-monophosphate (ara-CMP), an active metabolite of the nucleoside analog cytarabine formed by deoxycytidine kinase, is incorporated into DNA by DNA polymerase α, significantly slowing DNA synthesis. It inhibits nuclear and mitochondrial DNA replication in S. cerevisiae at 15 mM and improves survival in an L1210 murine leukemia model at 3.5-75.1 mg/kg.

Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg/ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg/ml, respectively). It also inhibits the growth of HeLa human cervical cancer cells (IC50 = 32 µg/ml) and reduces tumor growth in a murine L1210 lymphocytic leukemia model.

S-Adenosylhomocysteine (SAH) hydrolase is responsible for the reversible hydrolysis of SAH into adenosine and homocysteine. Inhibition of this enzyme leads to the accumulation of SAH within cells, thereby increasing the SAH to S-adenosylmethionine (SAM) ratio and subsequently inhibiting SAM-dependent methyltransferases. (−)-Neplanocin A, a potent and irreversible inhibitor of SAH hydrolase (Ki= 8.39 nM), exhibits significant antitumor activity against mouse leukemia L1210 cells and holds broad-spectrum antiviral properties. Its efficacy notably surpasses that of the reversible inhibitor 3-deazaneplanocin, especially in combating vesicular stomatitis, evidencing a higher potency with ID50 values of 0.07 μg/ml for Neplanocin A versus 0.3 μg/ml for 3-deazaneplanocin.

Raltitrexed (D1694)(IC50 of 9 nM), a thymidylate synthase inhibitor, is used for the inhibition of L1210 cell growth.

Urdamycin A is a bacterial metabolite originally isolated fromS. fradiaethat has antibacterial and anticancer activities.1,2It is active against a variety of Gram-positive and Gram-negative bacteria, includingB. subtilisand strains ofArthrobacterandStreptomyces, but not the fungusS. cerevisiae, in a disc assay when used at a concentration of 1 mg/ml.2Urdamycin A is cytotoxic to L1210 and HT-29, but not A549, cancer cells (IC50s = 7.5, 5, and >10 μg/ml, respectively).1

Homopteroic Acid is an intermediate in the synthesis of Homofolic Acid which inhibits the growth of L1210 mouse leukemia cells when intracellular folates are acquired via the high-affinity folate binding protein.

Bactobolin A, a microbial metabolite initially derived from Pseudomonas, exhibits both antibiotic and anticancer properties. It demonstrates activity against various bacteria including S. aureus, S. epidermidis, S. faecalis, B. anthracis, B. subtilis, E. coli, S. typhi, and S. dysenteriae, with minimum inhibitory concentrations (MICs) ranging from 0.1 to 12.5 µg/ml. Additionally, in vivo studies show that bactobolin A enhances survival rates at doses of 0.25 to 4 mg/kg in an L1210 murine leukemia model.

CI-898 HCl is a lipophilic antifolate inhibitor of dihydrofolate reductase (DHFR). It has enhanced binding to DHFR in the presence of the cofactor NADPH. Cl-898 HCl inhibits cell growth and halts the cell cycle at the G1/S phase in L1210 mouse lymphocytic leukemia cells and is active against methotrexate-resistant cancer cell lines. It also enhances the activity of doxorubicin, cyclophosphamide, and 6-thioguanine (6-TG) in mice with advanced stage P338 leukemia.

15-deoxy-Δ12,14-Prostaglandin D2 (15-deoxy-Δ12,14-PGD2) is a PGD2 metabolite functioning as an agonist for the PGD2 receptor 2 (DP2), with a binding affinity (Ki) of 50 nM for the mouse DP2 receptor expressed in HEK293 cell membranes. It activates eosinophils with an EC50 of 8 nM and enhances the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), initiating PPARγ-mediated transcription at 5 µM concentration. Furthermore, it exhibits cytotoxicity towards L1210 murine leukemia cells with an IC50 of 0.3 µg/ml and displays weaker inhibition of ADP-induced platelet aggregation than PGD2, with an IC50 of 320 ng/ml.

Acetomycin is a γ-lactone microbial metabolite originally isolated from S. ramulosus that has anticancer activity. It inhibits proliferation of HCT-8 human colon and L1210 mouse leukemia cancer cells.

11-epi-Chaetomugilin I, a metabolite identified in Chaetomium globosum, demonstrates notable cytotoxic activity against several cell lines, including the murine P388 and L1210 leukemia cell lines, the human HL-60 leukemia cell line, and the human KB epidermoid carcinoma cell line [1].

1-Methoxyphaseollidin exhibits anti-Helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains. 1-Methoxyphaseollidin may show moderate cytotoxic activity against KB and L1210 cells. 1-Methoxyphaseollidin also shows inhibition of lysoPAF acetyltransferase activity.

Santamarine has significant anticancer activity, can inhibit L1210 cells because of its cytotoxic,cytostatic and blocking mitosis and reducing uptake of thymidine. Santamarine and reynosin show bactericidal activity against clinical strains of Mycobacterium tuberculosis.

NU1064 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor, which can potentiate the cytotoxicity of a panel of mechanistically diverse anti-cancer agents in L1210 cells. NU1064 potentiated a sublethal concentration of a DNA methylating agent in a concentration-dependent manner.

Bisucaberin is a siderophore and bacterial metabolite that has been found inA. haloplanktisand has anticancer activity.1,2It inhibits the growth of L1210 and 1MC carcinoma cells (IC50s = 9.7 and 12.7 μM, respectively) and sensitizes fibrosarcoma 1023 cells to macrophage-mediated cytolysis. 1.Hou, Z., Raymond, K.N., O’Sullivan, B., et al.A preorganized siderophore: Thermodynamic and structural characterization of alcaligin and bisucaberin, microbial macrocyclic dihydroxamate chelating agentsInorg. Chem.37(26)6630-6637(1998) 2.Kameyama, T., Takahashi, A., Kurasawa, S., et al.Bisucaberin, a new siderophore, sensitizing tumor cells to macrophage-mediated cytolysis. I. Taxonomy of the producing organism, isolation and biological propertiesJ. Antibiot. (Tokyo)40(12)1664-1670(1987)

1,4-Anthraquinone is an anticancer drug that blocks nucleoside transport, inhibits macromolecule synthesis, induces DNA fragmentation, and decreases the growth and viability of L1210 leukemic cells in the same nanomolar range as daunorubicin in vitro.1,4-

Urdamycin B, an antibiotic derived from the metabolic products of Streptomyces fradiae, effectively inhibits fungi and bacteria, and exhibits anti-proliferative activity against mouse leukemia cells L1210. Its potential uses include research on cancer, bacterial, and fungal infections [1] [2].

Elliptinium acetate (NSC 264137), a DNA intercalating agent, exhibits high cytotoxicity towards L1210 cells and forms covalent bonds with nucleic acids from these cells. It holds potential in cancer research, especially for treating metastatic breast cancer.

5,2',6'-Trihydroxy-6,7,8-trimethoxyflavone (ED 50 =4.5 ug/ml ) shows cytotoxicity against L1210 cell and has inhibiting effects on ATPase from the cell.

8-Deazafolic acid is a potent folate-dependent bacteria inhibitor, Streptococcus faecium (ATCC 8043) and Lactobacillus casei (ATCC 7469), and to have activity against lymphoid leukemia L1210 in mice.

Altemicidin is a monoterpene alkaloid originally isolated from [S. sioyaensis] with acaricidal and anticancer activities. It is effective against two-spotted spider mites ([T. urticae]) in a greenhouse pot test at concentrations of 10 and 100 ppm. Altemicidin inhibits the growth of murine L1210 lymphocytic leukemia and IMC carcinoma cells (IC50s = 0.84 and 0.82 μg ml, respectively). It is toxic to mice with an LD50 value of 0.3 mg kg.

Thalidezine, a novel AMPK activator, eliminates apoptosis-resistant cancer cells through energy-mediated autophagic cell death, it can inhibit the growth of mouse L1210 cells in vitro. Thalidezine possesses antimicrobial activity against Mycobacterium sme

5'-Ethynyl-2'-deoxycytidine (EdC) functions as a nucleoside analog effectively inhibiting the replication of herpes simplex virus-1 (HSV-1) KOS strain with an ID50 of 0.2 μg/mL. Additionally, it decreases virus-induced cytopathogenic effects in PRK cells for HSV-1, HSV-2, and vaccinia virus strains, demonstrating MIC values between 0.2 to 5 μg/mL. EdC acts as a thymidylate synthetase inhibitor, selectively impacting the DNA incorporation rates of [1',2'-3H]deoxyuridine compared to [CH3-3H]deoxythymidine in PRK cells with ID50s of 3 and 120 μg/mL, respectively. It further inhibits thymidine synthetase and curtails L1210 cell proliferation, a process reversible by deoxythymidine (ID50s are 4.4 and 1,000 μg/mL, respectively). Also, EdC is utilized in monitoring DNA synthesis and cellular replication through click chemistry conjugation, linking its ethynyl group with the azido group of various fluorochromes.

Heliquinomycin is a bacterial metabolite originally isolated fromStreptomycesthat has diverse biological activities.1It is active against a variety of Gram-positive bacteria, including strains ofB. anthracis, B. subtilis, and methicillin-sensitive or -resistantS. aureus(MICs = <0.05-0.39 μg/ml). Heliquinomycin inhibits the activity of DNA helicase with a Kivalue of 6.8 μM. It reduces the growth of L1210 leukemia, B16 melanoma, and FS-3 fibrosarcoma cells (IC50s = 0.97, 0.89, and 0.83 μg/ml, respectively). 1.Chino, M., Nishikawa, K., Umekita, M., et al.Heliquinomycin, a new inhibitor of DNA helicase, produced by Streptomyces sp. MJ929-SF2 I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)49(8)752-757(1996)

Bruceantin (NSC-165563) is a natural product isolated from Brucea antidysenterica. Bruceantin has antitumor activity against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.