5969-92-6Relevant academic research and scientific papers
Benzimidazole ring-containing propyne amide derivative as well as preparation method and pharmaceutical composition and application thereof
-
Paragraph 0138-0140, (2020/11/13)
The invention relates to a benzimidazole ring-containing propiolamide derivative as shown in the formula I, its medicinal salt and their preparation method, a composition containing one or more of the compounds and an application of the compounds in treating tumor diseases.
Synthesis and biological evaluation of SANT-2 and analogues as inhibitors of the hedgehog signaling pathway
Buettner, Anita,Seifert, Katrin,Cottin, Thomas,Sarli, Vasiliki,Tzagkaroulaki, Lito,Scholz, Stefan,Giannis, Athanassios
experimental part, p. 4943 - 4954 (2009/12/24)
Hedgehog (Hh) signaling plays an important role in cell signaling of embryonic development and adult tissue homeostasis. In vertebrates, the hh gene encodes three different unique proteins: sonic hedgehog (Shh), desert hedgehog (Dhh) and indian hedgehog (Ihh). Disruption of the Hh signaling pathway leads to severe disorders in the development of vertebrates whereas aberrant activation of the Hh pathway has been associated with several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers. In vivo evidence suggests the antagonism of excessive Hh signaling provides a route to unique mechanism-based anti-cancer therapies. Recently the small molecule SANT-2 was identified as a potent antagonist of Hh-signaling pathway. Here, we describe the synthesis, SAR studies as well as biological evaluation of SANT-2 and its analogues. Fifteen SANT-2 derivatives were synthesized and analyzed for their interference with the expression of the Hh target gene Gli1 in a reporter gene assay. By comparison of structure and activity important molecular descriptors for Gli inhibition could be identified. Furthermore we identified derivative TC-132 that was slightly more potent than the parent compound SANT-2. Selected compounds were tested for Hh related teratogenic effects in the small teleost model medaka. Albeit Gli expression has indicated a 16-fold higher Hh-inhibiting activity than observed for the plant alkaloid cyclopamine, none of the tested compounds were able to induce the cyclopamine-specific phenotype in the medaka assay.
Zeolites. Efficient and eco-friendly catalysts for the synthesis of benzimidazoles
Heravi, Majid M.,Tajbakhsh, Mahmood,Ahmadi, Amir N.,Mohajerani, Bagher
, p. 175 - 179 (2007/10/03)
A superior method of synthesis of 2-substituted benzimidazoles by means of the heterogeneous catalysis of synthetic and natural zeolites in the reaction of 1,2-diaminobenzene with acid chlorides is described. Springer-Verlag 2005.
