Substituted tetrahydroisoquinolines as microtubule-destabilizing agents in triple negative human breast cancer cells was written by Gangapuram, Madhavi;Jean, Riccardo;Mazzio, Elizabeth;Badisa, Ramesh;Eyunni, Suresh;Goodman, Carl B.;Redda, Kinfe K.;Soliman, Karam F.. And the article was included in Anticancer Research in 2016.COA of Formula: C10H13ClO3S This article mentions the following:
Triple-neg. breast cancer (TNBC) occurs at greater frequency amongst African-Americans, being characterized by the absence of estrogen receptor (ER), progesterone receptor (PR) and human epidermal receptor 2 (HER2). TNBC is often invasive and typically treated with cytostatic agents such as taxanes in combination with anthracyclines or platinum-based drugs. In this study, we synthesized a number of tetrahydroisoquinoline moieties by N-amination of substituted isoquinolines by O-mesytelene sulfonylhydroxylamine followed by ylide formation and reduction, which yielded the desired, substituted tetrahydroisoquinolines (THIQs) in moderate to good yield. Using a differential scatter plot to identify potential selective ER-modulating drugs in ER-pos. control cells (MCF-7) driven by estradiol vs. TNBC (MDA-MB-231) cells, the in vitro data showed an absence of effects on the ER (compared to 4-hydroxytamoxifen and raloxifene). In contrast, two lead compounds halted proliferation (cytostatic) in MDA-MB-231 TNBC cells at a potency level below 2.5 μM concomitant with mitotic arrest, attenuated replicative DNA synthesis, halted microtubule nucleation/stunted tubulin polymerization, abnormal expansive cytoskeletal tubulin and actin morphologies with multinucleation of cells. The most effective cytostatic compounds GM-3-53 and GM-3-121 blocked replicative processes at the G2 growth phase. These findings suggest that specific THIQs work independently of the ER, by holding static the microtubule network thereby preventing mitosis. Future work is required to establish the safety and efficacy of these drugs and their potential adjunct therapeutic gain in the presence of taxanes in TNBC. In the experiment, the researchers used many compounds, for example, 4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3COA of Formula: C10H13ClO3S).
4-Butoxybenzene-1-sulfonyl chloride (cas: 1138-56-3) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.COA of Formula: C10H13ClO3S
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics