l1210

Procarbazine hydrochloride (NSC-77213 HCl) 是一种烷化剂，是甲基肼衍生物的盐酸盐，具有抗肿瘤和诱变活性。

Cyclophosphamide 是一种烷化剂，具有抗肿瘤及免疫抑制活性，用于治疗多种癌症。

Vancomycin 是一种糖肽类抗生素，可以通过改变细胞膜的渗透性并选择性地抑制核糖核酸的合成以发挥抗菌活性。Vancomycin 可以用于治疗所有抗生素均无效的严重感染。

Vancomycin hydrochloride (Vancomycin HCl) 是Vancomycin 的盐酸盐，是一种支链三环糖基化肽，对大多数生物体具有杀菌活性，对肠球菌具有抑菌作用。

Cytarabine (Ara-C) 是一种核苷类似物，一种 DNA 合成抑制剂 (IC50=16 nM)。Cytarabine 可以抑制 DNA 聚合酶，诱导细胞周期阻滞、细胞自噬和凋亡。Cytarabine 具有抗肿瘤活性。

5-Fluorouridine 是一种 5-fluorouracil 的代谢物，具有抗癌作用。它对 L1210 细胞的生长具有细胞毒性作用，其作用的 IC50值为 2 nM。它能抑制人结肠癌细胞 rRNA 的合成。

UNBS3157是一种新型的非血液毒性萘酰亚胺衍生物，具有强大的抗肿瘤活性，能够通过DNA插入作用和毒化拓扑异构酶IIalpha来与DNA结合。与之相关的萘酰亚胺类化合物Amonafide在二期乳腺癌试验中表现出了活性，但由于限制剂量的骨髓毒性，目前尚未进入三期临床试验。相比之下，UNBS3157的最大耐受剂量比Amonafide高出3-4倍，并且在显示出显著抗肿瘤效果的剂量下未引起小鼠的血液毒性。此外，在活体内模型中，包括(i) L1210鼠白血病、(ii) MXT-HI鼠乳腺腺癌、以及(iii)人类A549非小细胞肺癌和BxPC3胰腺癌原位模型中，UNBS3157显示出优于Amonafide的效果。

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 fromS. sioyaensiswith acaricidal and anticancer activities.1It is acaricidal to 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 LD50value of 0.3 mg kg. 1.Takahashi, A., Kurasawa, S., Ikeda, D., et al.Altemicidin, a new acaricidal and antitumor substance. I. Taxonomy, fermentation, isolation and physico-chemical and biological propertiesJ. Antibiot. (Tokyo)42(11)1556-1561(1989)

7-Ethylcamptothecin 是一种喜树碱类似物。其中喜树碱是一种细胞毒性生物碱，从喜树中分离出得到，对 L1210 白血病和 Walker 256 癌肉瘤模型具有很强的抗肿瘤活性。

4-Carboxyquinoline (4-Quinolinecarboxylic acid) 是内源性代谢产物的一种。

Raltitrexed (D1694) 是一种抗代谢药物，通过抑制胸苷酸合成酶起作用，可用于化疗。

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)为DNA插层剂，对L1210细胞显示出明显细胞毒性，并能与其核酸进行共价结合。该化合物主要用于癌症研究，特别是转移性乳腺癌。

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 是一种在Chaetomium globosum 中发现的代谢物。11-epi-Chaetomugilin I 对小鼠 P388 白血病细胞系、人类 HL-60 白血病细胞系、小鼠 L1210 白血病细胞系和人类 KB 表皮样癌细胞系具有显著的细胞毒性活性。

Podophyllotoxone 是从八角莲根中分离得到的一种天然产物，能抑制微管蛋白聚合，具有抗癌活性。

Bactobolin A 是一种最初从 Pseudomonas 中分离出的微生物代谢产物，具有抗生素和抗癌活性。它对 S. aureus、S. epidermidis、S. faecalis、B. anthracis、B. subtilis、E. coli、S. typhi 和 S. dysenteriae 活跃(MICs = 0.1-12.5 µg/ml)。在体内，bactobolin A (0.25-4 mg/kg) 提高了 L1210 小鼠白血病模型的存活率。