Category: indole-building-block. Authors Khedr, MA; Abu-Zied, KM; Zaghary, WA; Aly, AS; Shouman, DN; Haffez, H in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about in [Khedr, Mohammed A.; Zaghary, Wafaa A.] Helwan Univ, Fac Pharm, Dept Pharmaceut Chem, POB 11795, Cairo, Egypt; [Abu-Zied, Khadiga M.; Aly, Ahmed S.] Natl Res Ctr, Photochem Dept, Heterocycl Unit, Giza 12622, Egypt; [Shouman, Dina N.] Egyptian Minist Hlth & Populat, Family Med Ctr, Dakahlia, Egypt; [Haffez, Hesham] Helwan Univ, Fac Pharm, Biochem & Mol Biol Dept, POB 11795, Cairo, Egypt; [Haffez, Hesham] Helwan Univ, Ctr Sci Excellence Helwan Struct Biol Res HSBR, Cairo 11795, Egypt in 2021.0, Cited 96.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
There is a continuous need in drug development approach for synthetic anticancer analogues with new therapeutic targets to diminish chemotherapeutic resistance of cancer cells. This study presents new group of synthetic thienopyrimidine analogues (1-9) aims as mGluR-1 inhibitors with anticancer activity. In-vitro antiproliferative assessment was carried out using viability assay against cancer cell lines (MCF-7, A-549 and PC-3) compared to WI-38 normal cell line. Analogues showed variable anticancer activity with IC50 ranging from 6.60 to 121 mu g/mL with compound 7b is the most potent analogue against the three cancer cell lines (MCF-7; 6.57 +/- 0.200, A-549; 6.31 +/- 0.400, PC-3;7.39 +/- 0.500 mu g/mL) compared to Doxorubicin, 5-Flurouracil and Riluzole controls. Selected compounds were tested as mGluR-1 inhibitors in MCF-7 cell line and results revealed compound 7b induced significant reduction in extracellular glutamate release (IC50; 4.96 +/- 0.700 mu M) compared to other analogues and next to Riluzole (IC50; 2.80 +/- 0.500 mu M) of the same suggested mode of action. Furthermore, both cell cycle and apoptosis assays confirmed the potency of compound 7b for early apoptosis of MCF-7 at G2/M phase and apoptotic positive cell shift to (91.4%) compared to untreated control (19.6%) and Raptinal positive control (51.4%). On gene expression level, compound 7b induced over-expression of extrinsic (FasL, TNF-alpha and Casp-8), intrinsic (Cyt-C, Casp-3, Bax) apoptotic genes with down-regulation of anti-apoptotic Bcl-2 gene with boosted Bax/Bcl-2 ratio to 2.6-fold increase. Molecular docking and dynamic studies confirmed the biological potency through strong binding and stability modes of 7b where it was faster in reaching the equilibrium point and achieving the stability than Riluzole over 20 ns MD. These results suggest compound 7b as a promising mGluR inhibitory scaffold with anticancer activity that deserves further optimization and in-depth In-vivo and clinical investigations.
About 4-Methoxybenzaldehyde, If you have any questions, you can contact Khedr, MA; Abu-Zied, KM; Zaghary, WA; Aly, AS; Shouman, DN; Haffez, H or concate me.. Category: indole-building-block
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles