l1210

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.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Vancomycin is a glycopeptide antibiotic that exerts its antibacterial activity by inhibiting the second stage of cell wall synthesis in susceptible bacteria. It also alters cell membrane permeability and selectively inhibits RNA synthesis. Vancomycin is commonly used to treat severe infections resistant to other antibiotics and is frequently employed in experimental studies to induce kidney injury models.

Vancomycin hydrochloride (Vancomycin HCl) is a glycopeptide antibiotic that targets Peptidoglycan in bacterial cell wall synthesis. Vancomycin hydrochloride is mainly used for the treatment of severe Gram-positive bacterial infections.

Cytarabine (Ara-C) is a nucleoside analog, an inhibitor of DNA synthesis (IC50=16 nM). Cytarabine inhibits DNA polymerase and induces cell cycle arrest, autophagy, and apoptosis. Cytarabine has antitumor activity.

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.

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.

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-

UNBS3157 is a novel naphthalimide derivative that is non-hematotoxic and exhibits significant antitumor activity through DNA intercalation and the poisoning of topoisomerase IIalpha. Unlike Amonafide, a related naphthalimide compound that showed activity in Phase II breast cancer trials but did not proceed to Phase III due to dose-limiting myelotoxicity, UNBS3157 has a maximum tolerated dose 3-4 times higher and does not cause hematotoxicity in mice at effective antitumor doses. In vivo models, including (i) L1210 mouse leukemia, (ii) MXT-HI mouse mammary adenocarcinoma, and (iii) human A549 non-small cell lung carcinoma and BxPC3 pancreatic cancer orthotopic models, demonstrate superior efficacy of UNBS3157 compared to Amonafide.

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.

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

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)

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)

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.

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

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

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.

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.

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.

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.

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.

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.

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].

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