cross-resistance

Amcenestrant (SAR439859) 是一种有效的 ER 拮抗剂，具有 ER 降解活性，EC50为 0.2 nM。它是一种具有口服活性，非甾体和选择性雌激素受体降解剂 (SERD)。它可在 ER+乳腺癌中表现出强大的抗肿瘤功效和有限的交叉耐药性。

Spirodiclofen (BAJ-2740) 是选择性非系统性的杀螨剂，来自新的化学类特酮酸衍生物， 与目前市面上的杀螨剂无交叉耐药, 具有额外的杀虫性能。

MBX-1162，一种双吲哚类化合物，研究显示，在金黄色葡萄球菌的耐药机制中，没有与其他相关化合物展现交叉耐药性，这与其对MepA和MepR的底物特异性相关。

Lenacapavir，又名GS-6207，是一种HIV-1 capsid抑制剂。其对23种来自不同亚型的HIV-1临床分离株表现出平均EC50为50 pM (20-160 pM)，这些测试是在周围血单核细胞（PBMCs）中进行的。Lenacapavir在体外显示出皮克摩尔级的有效性，且对现有抗逆转录病毒类化合物没有交叉抗性。此外，在HIV-1感染者中，Lenacapavir展现出强大的抗病毒活性，无论治疗历史如何，都没有发现对Lenacapavir的预存在抗性。

Picoplatin has a broad spectrum of antineoplastic activity and is designed to overcome platinum drug resistance. Picoplatin alkylates DNA, forming both intra- and inter-strand cross-linkages, resulting in the inhibition of DNA replication and transcriptio

Lascufloxacin (KRP-AM-1977) is a potent antibacterial drug candidate. It exhibited the most potent activity against gram-positive bacteria among the quinolones tested. Lascufloxacin showed incomplete cross-resistance against existing quinolone-resistant s

Platencin is a natural, broad spectrum Gram-positive antibiotic isolated from S. platensis, which is also the source of platensimycin . Platencin inhibits two key enzymes in bacterial fatty acid synthesis, β-ketoacyl-ACP synthases II and III (FabF and FabH, respectively), unlike platensimycin which only targets FabF. The IC50 values for platencin against FabF and FabH are 1.95 and 3.91 μg ml, respectively. It does not exhibit cross-resistance to antibiotic resistant bacterial strains, including methicillin-resistant S. aureus, vancomycin-intermediate S. aureus, and vancomycin-resistant Enterococci. For these reasons, platencin has potential applications in fighting antibiotic resistant bacteria.

S-MGB-234 is a minor groove binder utilized for the treatment of Animal African Trypanosomiasis (AAT). It exhibits exceptional in vitro efficacy against the primary causative agents of AAT, namely Trypanosoma congolense and Trypanosoma vivax. Moreover, S-MGB-234 does not demonstrate cross-resistance with existing diamidine drugs and is not internalized through the transporters employed by diamidines.

Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of

Pyraziflumid is a fungicide. Pyraziflumid is a novel member of succinate dehydrogenase inhibitor fungicides (SDHI). The average EC50 value was 0.0561 (±0.0263)μg ml for mycelial growth. There was no cross-resistance between pyraziflumid and the widely used fungicides carbendazim, dimethachlon and the phenylpyrrole fungicide fludioxonil.

Albizziin is amino acid analog which acts as a competitive inhibitor of asparagine synthetase with respect to glutamine. Albizziin has been used to isolate mutants of Chinese hamster ovary cells with alterations in levels of the target enzyme. Several classes of mutations can be distinguished on the basis of cross-resistance to beta-aspartyl hydroxamate, another amino acid analog. Studies on asparagine synthetase indicate that resistance to albizziin may be due to altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification.

NVR 3-778 is the first capsid assembly modulator (CAM) that has demonstrated antiviral activity in hepatitis B virus (HBV)-infected patients. NVR 3-778 inhibited the generation of infectious HBV DNA-containing virus particles with a mean antiviral 50% effective concentration (EC50) of 0.40 µM in HepG2.2.15 cells. The antiviral profile of NVR 3-778 indicates pan-genotypic antiviral activity and a lack of cross-resistance with nucleos(t)ide inhibitors of HBV replication.

Ibrexafungerp citrate is a triterpenoid antifungal. Similarly to echinocandins, it inhibits the synthesis of 1,3-β-d-glucan. However, it binds to a different site on the enzyme than echinocandins, resulting in limited cross-resistance. Ibrexafungerp exerts concentration-dependent fungicidal activity against Candida species and retains in vitro activity against most fluconazole-resistant strains.

Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerated and more effective at inhibiting tumor growth compared with mitoxantrone in a human xenograft tumor regression mouse model. Mechanistically, we found that ethonafide inhibited topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIalpha and -beta. In addition, ethonafide induced a potent G(2) cell cycle arrest in the DU 145 human prostate cancer cell line. By creating stable cell lines with decreased expression of topoisomerase IIalpha or -be......

(6R)-ML753286 是 ML753286 的异构体。ML753286 是一种口服活性和选择性 BCRP(抗乳腺癌蛋白) 抑制剂，IC50为 0.6 μM。 ML753286 在啮齿动物和人类肝脏 S9 组分中具有高渗透性和低至中等清除率，并且在不同物种中都具有血浆稳定性。

Pentaerythritol tetra(3-mercaptopropionate) 是一种含有季戊四醇和巯基丙酸酯基团的有机化合物。它在多种化学和工业领域中被用作稳定剂和交联剂。其特性包括增强聚合物与涂料的机械强度、热稳定性及耐候性。此外，它还可作为生产其他特种化学品和材料的原料。