ChemInform Abstract: ALKYLATED 5‐FLUOROURACILS AS ANTICANCER AGENTS

Sanyal, Utpal; Dutta, Subhabrata; Banerjee, S.; Chakraborti, S. K.

doi:10.1002/chin.198301266

Cited by 1 publication

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“…Synthesis of a number of drug candidates bearing this functionality has been reported [3-5 (and references cited therein)]. As a part of our anticancer drug development programme [6][7][8], we have synthesised [9] some suitably sub stituted nucleic acid bases bearing the a-methylene-y-lactone moiety as poten tial anticancer agents (figure 1) and these were screened for their in vivo anti tumour activity against Ehrlich as cites carcinoma in Swiss mice and in few cases against PS and KB cells [9], Some of the derivatives showed significant anti tumour activity in vitro and in vivo. The present study is an approach to cor relate the effect of these compounds on transcription and translation for evalua tion of their biochemical mechanism of action.…”

Section: Introductionmentioning

confidence: 99%

Mechanism of Action of Alpha-Methylene-Gamma-Lactone Derivatives of Substituted Nucleic Acid Bases in Tumour Cells

Panda¹,

Choudhury²,

Sanyal

et al. 1989

Chemotherapy

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Some α-methylene-γ-lactone derivatives of substituted nucleic acid bases, which showed significant antitumour activity against experimental tumours, were tested for their possible mechanism of action. Derivatives 1, 4 and 7 strongly inhibit active transport of uridine through sarcoma-180 ascites tumour cells. Derivatives 1, 7 and 10 strongly inhibit a translation process in these cells, besides apparent inhibition in transcription. It appears that active transport and translation might be the primary steps inhibited by these drugs.

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Section: Introductionmentioning

confidence: 99%