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Design and Synthesis of Novel 2-Acetamido, 6-Carboxamide Substituted Benzothiazoles as Potential BRAFV600E Inhibitors – In vitro Evaluation of their Antiproliferative Activity
ChemMedChem ( IF 3.6 ) Pub Date : 2023-10-04 , DOI: 10.1002/cmdc.202300322 Yakinthi Batsi 1 , Georgia Antonopoulou 1 , Theano Fotopoulou 1 , Kassandra Koumaki 1 , Eftichia Kritsi 1 , Constantinos Potamitis 1 , Maria Goulielmaki 1 , Salomi Skarmalioraki 1 , Chara Papalouka 1 , Eleni Poulou-Sidiropoulou 1 , Vivian Kosmidou 1 , Stavroula Douna 1 , Maria-Sofia Vidali 1 , Eleni-Fani Gkotsi 1 , Aristotelis Chatziioannou 1 , Vassilis L Souliotis 1 , Vasiliki Pletsa 1 , Olga Papadodima 1 , Vassilis Zoumpourlis 1 , Panagiotis Georgiadis 1 , Maria Zervou 1 , Alexander Pintzas 1 , Ioannis D Kostas 1
ChemMedChem ( IF 3.6 ) Pub Date : 2023-10-04 , DOI: 10.1002/cmdc.202300322 Yakinthi Batsi 1 , Georgia Antonopoulou 1 , Theano Fotopoulou 1 , Kassandra Koumaki 1 , Eftichia Kritsi 1 , Constantinos Potamitis 1 , Maria Goulielmaki 1 , Salomi Skarmalioraki 1 , Chara Papalouka 1 , Eleni Poulou-Sidiropoulou 1 , Vivian Kosmidou 1 , Stavroula Douna 1 , Maria-Sofia Vidali 1 , Eleni-Fani Gkotsi 1 , Aristotelis Chatziioannou 1 , Vassilis L Souliotis 1 , Vasiliki Pletsa 1 , Olga Papadodima 1 , Vassilis Zoumpourlis 1 , Panagiotis Georgiadis 1 , Maria Zervou 1 , Alexander Pintzas 1 , Ioannis D Kostas 1
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Eleven new substituted benzothiazole derivatives were designed and synthesized in order to provide efficient inhibitors of the oncogenic BRAFV600E kinase. They were biologically evaluated as potential BRAFV600E inhibitors, MEK-ERK pathway inhibitors and antiproliferative agents in several colorectal cancer and melanoma cell lines. In all assays applied, the analog 2-acetamido-N-[3-(pyridin-2-ylamino)propyl]benzo[d]thiazole-6-carboxamide (22) provided promising results in view of its use in drug development.
中文翻译：
作为潜在 BRAFV600E 抑制剂的新型 2-乙酰氨基、6-甲酰胺取代苯并噻唑的设计和合成 – 其抗增殖活性的体外评价
设计并合成了11 种新的取代苯并噻唑衍生物，以提供致癌 BRAFV600E 激酶的有效抑制剂。它们在多种结直肠癌和黑色素瘤细胞系中被生物学评估为潜在的 BRAFV600E 抑制剂、MEK-ERK 通路抑制剂和抗增殖剂。在所有应用的测定中，类似物2-乙酰氨基-N- [3-(吡啶-2-基氨基)丙基]苯并[d]噻唑-6-甲酰胺( 22 )鉴于其在药物开发中的用途提供了有希望的结果。
更新日期：2023-10-04
中文翻译：
作为潜在 BRAFV600E 抑制剂的新型 2-乙酰氨基、6-甲酰胺取代苯并噻唑的设计和合成 – 其抗增殖活性的体外评价
设计并合成了11 种新的取代苯并噻唑衍生物，以提供致癌 BRAFV600E 激酶的有效抑制剂。它们在多种结直肠癌和黑色素瘤细胞系中被生物学评估为潜在的 BRAFV600E 抑制剂、MEK-ERK 通路抑制剂和抗增殖剂。在所有应用的测定中，类似物2-乙酰氨基-N- [3-(吡啶-2-基氨基)丙基]苯并[d]噻唑-6-甲酰胺( 22 )鉴于其在药物开发中的用途提供了有希望的结果。
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