关键词: cancer hybrid molecules mechanisms of action pyrimidine quinazoline structure–activity relationship sulfonamide

Mesh : Humans Sulfonamides / chemistry pharmacology chemical synthesis Pyrimidines / chemistry pharmacology chemical synthesis Antineoplastic Agents / pharmacology chemistry chemical synthesis Neoplasms / drug therapy pathology Carbonic Anhydrase Inhibitors / chemistry pharmacology chemical synthesis Molecular Structure Animals

来  源:   DOI:10.4155/fmc-2024-0010

Abstract:
Cancer as a devastating malignancy, seriously threatens human life and health, but most chemotherapeutics have long been criticized for unsatisfactory therapeutic efficacy due to drug resistance and severe off-target toxicity. Pyrimidines, including fused pyrimidines, are privileged scaffolds for various biological cancer targets and are the most important class of metalloenzyme carbonic anhydrase inhibitors. Pyrimidine-sulfonamide hybrids can act on different targets in cancer cells simultaneously and possess potent activity against various cancers, revealing that hybridization of pyrimidine with sulfonamide is a promising approach to generate novel effective anticancer candidates. This review aims to summarize the recent progress of pyrimidine-sulfonamide hybrids with anticancer potential, covering papers published from 2020 to present, to facilitate further rational design of more effective candidates.
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摘要:
癌症是一种毁灭性的恶性肿瘤,严重威胁人类生命和健康,但由于耐药性和严重的脱靶毒性,大多数化疗药物长期以来一直被批评为疗效不理想。嘧啶,包括稠合嘧啶,是各种生物癌症靶标的特权支架,并且是最重要的金属酶碳酸酐酶抑制剂。嘧啶-磺酰胺杂种可以同时作用于癌细胞中的不同靶标,并具有针对各种癌症的有效活性。揭示嘧啶与磺酰胺的杂交是产生新的有效抗癌候选物的有希望的方法。本综述旨在总结嘧啶磺酰胺杂种具有抗癌潜力的最新进展。涵盖2020年至今发表的论文,便于进一步合理设计更有效的候选人。
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