An article Design, synthesis and anticervical cancer activity of new benzofuran-pyrazol-hydrazono- thiazolidin-4-one hybrids as potential EGFR inhibitors and apoptosis inducing agents WOS:000476615700014 published article about GROWTH-FACTOR RECEPTOR; MOLECULAR DOCKING; KINASE INHIBITORS; BREAST-CANCER; IN-VITRO; DERIVATIVES; ANTICANCER; DISCOVERY in [Abbas, Hebat-Allah S.] King Khalid Univ, Coll Sci, Chem Dept, Abha, Saudi Arabia; [Abbas, Hebat-Allah S.] Natl Res Ctr, Photochem Dept, Cairo 12622, Egypt; [Abd El Karim, Somaia S.] Natl Res Ctr, Dept Therapeut Chem, Cairo 12622, Egypt in 2019.0, Cited 35.0. Formula: C9H10O3. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7
This study represents the synthetic approaches of a new set of 2-(((3-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-4-yemethylene)hydrazono)-5-(aryl)thiazolidin-4-one derivatives 4-22 aiming to obtain new antiproliferative candidates against human cervix carcinoma cells (Hela) of EGFR PK inhibiting potency. The cancer cells represented promising sensitivity towards the compounds 6, 7, 11, 13, 14, 16, 17 more than or equal to that against the reference drug doxorubicin. In addition, the latter compounds were tested as EGFR protein kinase inhibitors. The results revealed that compound 14 showed more significant EGFR PK inhibitory activity than the reference drug erlotinib (IC50; 0.07, 0.08 mu M, respectively). Moreover, cell cycle analysis and apoptosis assay were performed for compound 14 proving its ability to cause G1/S phase arrest and apoptosis in Hela cancer cells, in addition to its activation of the caspases-7 and -3. In addition, derivative 14 increased the expression level of p53 and the ratio of Bax/Bcl-2 which confirmed its mode of action. Molecular docking study of 14 was performed to investigate its binding mode of interaction with EGFR PK in the active site with the aim of rationalizing its promising inhibitory activity. Accordingly, compound 14 might be considered as a promising scaffold anticervical cancer chemotherapeutic and deserves further optimization and in-depth biological studies.
Formula: C9H10O3. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Abbas, HAS; Abd El Karim, SS or concate me.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com