Recently I am researching about ANTIPROLIFERATIVE ACTIVITY; DRUG DISCOVERY; DESIGN; EXPRESSION; MECHANISM; MOIETIES; GROWTH; ASSAY; PANEL, Saw an article supported by the Deanship of Scientific Research at King Saud UniversityKing Saud University [RG-1439-65]. Published in ACADEMIC PRESS INC ELSEVIER SCIENCE in SAN DIEGO ,Authors: Eldehna, WM; Abdelrahman, MA; Nocentini, A; Bua, S; Al-Rashood, ST; Hassan, GS; Bonardi, A; Almehizia, AA; Alkahtani, HM; Alharbi, A; Gratteri, P; Supuran, CT. The CAS is 93-02-7. Through research, I have a further understanding and discovery of 2,5-Dimethoxybenzaldehyde. Product Details of 93-02-7
In the presented work, we report the synthesis of a series of 4-benzylidene-2-phenyl-5(4H)-imidazolone-based benzenesulfonamides 7a-f via the Erlenmeyer-Plochl reaction. All the prepared imidazolones 7a-f were evaluated as inhibitors of human (h) carbonic anhydrases (CA, EC 4.2.1.1) cytosolic isoforms hCA I and II, as well as transmembrane tumor-associated isoforms hCA IX and XII. All the tested hCA isoforms were inhibited by the prepared imidazolones 7a-f in variable degrees with the following KIs ranges: 673.2-8169 nM for hCA I, 61.2-592.1 nM for hCA II, 23-155.4 nM for hCA XI, and 21.8-179.6 nM for hCA XII. In particular, imidazolones 7a, 7e, and 7f exhibited good selectivity towards the tumor-associated isoforms (CAs IX and XII) over the off-target cytosolic (CAs I and II) with selectivity index (SI) in the range of 6.2-19.4 and 3.3-8, respectively. Moreover, imidazolones 7a-f were screened for their anticancer activity in one dose (10(-5) M) assay against a panel of 60 cancer cell lines according to US-NCI protocol. Furthermore, 7a, 7e and 7f were evaluated for their anti-proliferative activity against colorectal cancer HCT-116 and breast cancer MCF-7 cell lines. Furthermore, 7e and 7f were screened for cell cycle disturbance and apoptosis induction in HCT-116 cells. Finally, a molecular docking study was carried out to rationalize the obtained results.
Product Details of 93-02-7. About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Eldehna, WM; Abdelrahman, MA; Nocentini, A; Bua, S; Al-Rashood, ST; Hassan, GS; Bonardi, A; Almehizia, AA; Alkahtani, HM; Alharbi, A; Gratteri, P; Supuran, CT or concate me.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com