Optically active 1,3,4,4-tetrasubstituted beta-lactams: synthesis and evaluation as tumor cell growth inhibitors.

Perez Faginas P; Aranda MT; Garcia Lopez MT; Francesch A; Cuevas C; Gonzalez Muniz R

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Optically active 1,3,4,4-tetrasubstituted beta-lactams: synthesis and evaluation as tumor cell growth inhibitors.

机译：光学活性的1,3,4,4-四取代的β-内酰胺类化合物：作为肿瘤细胞生长抑制剂的合成和评估。

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The in vitro cytotoxicity assays of several enantiopure (3S,4S)- and (3R,4R)-1,3,4,4-tetrasubstituted beta-lactams derived from amino acids have shown that the (3S,4S)-4-benzyl-1-p-methoxybenzyl-3-methyl-4-methoxycarbonyl derivative 2a, obtained from Phe, displays significant activity, which is comparable to that of the anticancer drug Doxorubicin against HT29 cell lines. Modifications at positions 1 and 4 of the beta-lactam ring led to identify the Tyr(2,6-ClBz) analogu 26d with similar activity data to those of 2a. The synthesis and SAR of all these tetrasubstituted beta-lactams are reported here.

机译：几种源自氨基酸的对映体（3S，4S）-和（3R，4R）-1,3,4,4-四取代的β-内酰胺的体外细胞毒性试验表明，（3S，4S）-4-苄基从Phe获得的-1-对甲氧基苄基-3-甲基-4-甲氧基羰基衍生物2a显示出显着的活性，这与抗癌药物阿霉素对HT29细胞系的活性相当。 β-内酰胺环的位置1和4的修饰导致鉴定出具有与2a类似的活性数据的Tyr（2,6-ClBz）类似物26d。本文报道了所有这些四取代的β-内酰胺的合成和SAR。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第10期|共12页
作者
Perez Faginas P; Aranda MT; Garcia Lopez MT; Francesch A; Cuevas C; Gonzalez Muniz R;
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1. Optically active 1,3,4,4-tetrasubstituted beta-lactams: synthesis and evaluation as tumor cell growth inhibitors. [J] . Perez Faginas P, Aranda MT, Garcia Lopez MT, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第10期

机译：光学活性的1,3,4,4-四取代的β-内酰胺类化合物：作为肿瘤细胞生长抑制剂的合成和评估。
2. Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent. [J] . Li Qun, bbott.com, Woods KeithW, Bioorganic and Medicinal Chemistry Letters . 2002,第3期

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机译：Thieno [3,2-b]吡啶系列中的氨基二（杂）芳基胺：合成，对人类肿瘤细胞生长的影响，细胞周期分析，凋亡以及使用非肿瘤细胞的毒性评估

Optically active 1,3,4,4-tetrasubstituted beta-lactams: synthesis and evaluation as tumor cell growth inhibitors.

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