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Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFR^WT and EGFR^T790M: integrating biological, molecular docking, and ADMET analysis.

ABSTRACT: A series of derivatives (5-14) were synthesized through the diazotization of sulfadiazine with active methylene compounds. The chemical structures of these newly designed compounds were validated through spectral and elemental analysis techniques. The antiproliferative potential of derivatives 5-14 was assessed against three distinct cancer cell lines (A431, A549, and H1975) using the MTT assay. The results revealed that compounds 8, 12, and 14 exhibited the most potent antiproliferative activity, with IC₅₀ values ranging from 2.31 to 7.56 μM. Notably, these values were significantly lower than those of known EGFR inhibitors, including erlotinib, gefitinib, and osimertinib, suggesting the potential of these derivatives as novel antiproliferative agents. Furthermore, compound 12

SUBMITTER: Abd El-Lateef HM

PROVIDER: S-EPMC11378702 | biostudies-literature | 2024 Sep

REPOSITORIES: biostudies-literature

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Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFR^WT and EGFR^T790M: integrating biological, molecular docking, and ADMET analysis.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFRWT and EGFRT790M: integrating biological, molecular docking, and ADMET analysis.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Design and evaluation of sulfadiazine derivatives as potent dual inhibitors of EGFR^WT and EGFR^T790M: integrating biological, molecular docking, and ADMET analysis.