analogues

SK33 是一种有效的组织选择性抗雄激素药物，是一种肌醇类似物，能够降低雄激素受体 (AR) 的转录活性。

3-Amino-1-(2-chloro-10H-phenothiazin-10-yl)-1-propanone 参与而合成吩噻嗪系列化合物。

MLN9708 (Ixazomib Citrate) 抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点 (Ki50=0.93 nM, IC50=3.4 nM/)。 MLN9708 的生物活性形式是水溶液或血浆中的 MLN2238。

Clozapine Analogues 可用于研究神经系统疾病。

CP 866087 是一种阿片受体拮抗剂，可用于研究女性性功能障碍。

A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.

α-(difluoromethyl)-DL-Arginine (RMI 71897) 是一种酶激活的、不可逆的大肠杆菌(Ki = 800 μM)、铜绿假单胞菌和肺炎克雷伯菌精氨酸脱羧酶抑制剂。在0.01 mM 时，它已被证明可以防止渗透胁迫诱导的燕麦叶片细胞精氨酸脱羧酶活性和腐胺合成的增加。当α-(difluoromethyl)-DL-Arginine 与多种多胺类似物联用时，能在10 mM 的最低浓度下抑制克氏锥虫在哺乳动物宿主细胞中的生长，并在T 细胞受体α缺陷小鼠模型中阻止小锥虫的生长。

BTA-188是一种新型的和具有口服活性的合成的苯并恶唑和苯并噻唑衍生物中有效的类似物 ，具有显著抗鼻病毒活性 。

Gamibetal (4-Amino-3-hydroxybutyric Acid) 是 γ-氨基-β-羟基丁酸，对癫痫具有潜在的研究价值。

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。

COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。

Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities. Ecteinascidin-Analog-1 is a useful intermediate for chemical sythesis of Ecteinascidin analogues.

DBCO-C6-acid is a non-cleavable linker utilized for the synthesis of antibody-drug conjugates (ADCs) and carmaphycin analogues[1].

PF-06380101 is an auristatin microtubule inhibitor and is a cytotoxic Dolastatin 10 analogue. When compared to other synthetic auristatin analogues that are used in the preparation of ADCs, PF-06380101 displays excellent potencies in tumor cell proliferat

ATP-polyamine-biotin is a cell-permeable, efficient kinase cosubstrate with conversions and kinetics similar to those of other known ATP analogues. APB shows a cytotoxicity EC50 value of 19 ± 1 mM. ATP-polyamine-biotin is shown to promote biotin labeling

2-(Dimethylamino)acetaldehyde hydrochloride can be used to synthesis Muscarine analogues.

2-(Dimethylamino)acetaldehyde can be used to synthesis Muscarine analogues.

Endochin is an experimental antimalarial. Endochin and analogues thereof are causal prophylactic and potent erythrocytic stage agents in avian models.

S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and persistent histone gamma-H2AX. The chem

(+) - cloprostenol sodium is a kind of water-soluble prostaglandin F2 α ( PGF2 α) Analogues. It is an FP receptor agonist and a potent luteinizing agent in rats and hamsters.

Juvabione is the methyl ester of todomatuic acid, both of which are sesquiterpenes (C15) found in the wood of true firs of the genus Abies. They exist as part of a mixture of sesquiterpenes based on the bisabolane scaffold. Sesquiterpenes of this family,

(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 |1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).|2. Ayers, S., Graf, T.N., Adcock, A.F., et al. Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)