What question did this study set out to answer?

This research aims to synthesize and evaluate quinoxaline derivatives for their anticancer properties. The study specifically investigates their growth inhibition effects on cancer cell lines.

April 27, 2026Open Access

Quinoxaline chemistry. Part 11. 3-phenyl-2phenoxy- and phenoxymethyl-6(7) or 6,8-substituted quinoxalines and N-4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethylbenzoylglutamates. Synthesis and evaluation of in

Key Points

This research aims to synthesize and evaluate quinoxaline derivatives for their anticancer properties. The study specifically investigates their growth inhibition effects on cancer cell lines.
Twenty-four quinoxaline derivatives were screened for anticancer activity at National Cancer Institute.
In vitro tumor growth inhibition was assessed at various concentrations (10(-4) M to 10(-8) M).
Enzymatic activity against dihydrofolate reductase was evaluated for the most active compounds.
Ten quinoxaline derivatives showed significant tumor growth inhibition at 10(-4) M concentration in all cancer cell lines.
Four compounds maintained inhibitory activity significantly at 10(-5) M concentration.
Dihydrofolate reductase activity was appreciable for these quinoxalines in comparison to previously described aza analogues.

Abstract

Twenty-four out of twenty-nine quinoxalines were selected at the National Cancer Institute, Bethesda, Md, USA, for in vitro anticancer screening. Among these, 10 derivatives exhibited high values of percent tumor growth inhibition at a concentration of 10(-4) M in all cancer cell lines. Four of these compounds maintained these values at 10(-5) M, whereas a certain number exhibited significant values of percent inhibition at the most diluted concentrations (10(-8)-10(-6) M). Inhibitory activity against dihydrofolate reductase (DHFR) (bovine and rat liver) was determined for the most active compounds. This test showed that this type of quinoxaline exhibited an appreciable activity in comparison with the previously described aza analogues. In the other test (Lactobacillus casei, thymidylate synthase (TS), human HTS) no or poor activity was detected in both series of compounds. (C) 1998 Elsevier Science S.A. All rights reserved.

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Cite This Study

P et al. (Thu,) studied this question.

synapsesocial.com/papers/69eefcf4fede9185760d3bc8 https://doi.org/https://doi.org/10.1016/s0014-827x(98)00054-6

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