An article Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol WOS:000612171500005 published article about PHOSPHONIUM SALTS in [Pugachev, Mikhail, V; Pavelyev, Roman S.; Nguyen, Thang N. T.; Gabbasova, Raylya R.; Bulatov, Timur M.; Iksanova, Alfiya G.; Aljondi, Bashar; Bondar, Oksana, V; Grishaev, Denis Yu; Nikishova, Tatyana, V; Balakin, Konstantin, V; Shtyrlin, Yurii G.] Kazan Volga Reg Fed Univ, Kremlyovskaya 18, Kazan 420008, Russia; [Yamaleeva, Zilya R.; Kataeva, Olga N.] RAS, AE Arbuzov Inst Organ & Phys Chem, FRC Kazan Sci Ctr, Arbuzov Str 8, Kazan 420088, Russia in 2021.0, Cited 26.0. Computed Properties of C9H10O3. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9
A new efficient approach to the synthesis of 6-alkenyl substituted pyridoxine derivatives has been developed. A series of 31 novel alkenyl pyridoxine derivatives, stilbene-based bioisosteric analogs of estradiol, were synthesized. In vitro cytotoxicity of the obtained compounds against MCF-7 (ER+) breast cancer tumor cells was studied using the MTT assay. The most active compounds with IC50, MCF-7 < 10 mu M were also tested for cytotoxicity in vitro against MDA-MB-231 (ER-) breast adenocarcinoma cells and conditionally normal human skin fibroblasts (HSF). The patterns of structure-antitumor activity relationships of the obtained compounds were analyzed. The most active compounds were found to contain a six-membered ketal ring, a methyl group in position 5, a 3,4-dimethoxystyryl fragment in positions 2 or 6 of the pyridoxine ring, and a trans-configuration of the double bond. Using the most active compound 5a as a representative cytotoxic agent, we have demonstrated that it has high specificity and antiproliferative activity against MCF-7 (ER+) tumor cells (IC50 < 5 mu M), and a higher therapeutic index compared to the reference compound raloxifene (48 versus 5.8). Compound 5a decreased the mitochondrial membrane potential and increased the level of reactive oxygen species in MCF-7 cells, but not MDA-MB-231 cells. Compound 5a did not affect the distribution of cell cycle phases and induced apoptosis in MCF-7 cells, but not MDA-MB-231. Unlike compound 5a, raloxifene decreased mitochondrial potential, increased the ROS level, and induced apoptosis in both MCF-7 and MDA-MB-231 cells, which indicated a lack of selectivity for cells with estrogen receptor expression. It was also shown that compound 5a reduced the level of ER alpha expression in cells to a lesser extent than raloxifene and, unlike the latter, did not activate the PI3K/Akt signaling pathway. Computed Properties of C9H10O3. Welcome to talk about 120-14-9, If you have any questions, you can contact Pugachev, MV; Pavelyev, RS; Nguyen, TNT; Gabbasova, RR; Bulatov, TM; Iksanova, AG; Aljondi, B; Bondar, OV; Grishaev, DY; Yamaleeva, ZR; Kataeva, ON; Nikishova, TV; Balakin, KV; Shtyrlin, YG or send Email.
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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