Natural product-inspired rational design, synthesis and biological evaluation of 2,3-dihydropyrano[2,3- f ]chromen-4(8 H )-one based hybrids as potential mitochondrial apoptosis inducers

New chromanone derivatives containing thiazoles: Synthesis and antitumor activity evaluation on A549 lung cancer cell line

“…Bcl‐2 proteins have both proapoptotic (Bax, Bak, Bad, Bcl‐Xs, Bid, Bik Bim, and Hrk) and antiapoptotic (Bcl‐2, Bcl‐X L , Bcl‐W, Bfl‐2, and Mcl‐1) functions and play an important role in the intrinsic apoptotic pathway. Bcl‐2 family members are central regulatory proteins in the intrinsic mitochondrial apoptotic program and their interactions determine whether the cell will undergo apoptosis (Sakthivel et al, 2016). After 24 h of treatment of A549 cells with compounds 2b , 2c , and 2g at their IC 50 concentration, expression levels of Bcl‐2 and Bax were determined by immunohistochemical staining.…”

“…The compounds were studied at 100 μg/mL and exhibited inhibition in between 6.43% and 44.64%. mine whether the cell will undergo apoptosis (Sakthivel et al, 2016).…”

Crystal structure and Hirshfeld surface analysis of 5-(5-phenyl-1,2-oxazol-3-yl)-1,3,4-thiadiazol-2-amine

“…There are many approaches for building a thiadiazole heterocycle based on the use of carboxylic acids (Bhinge et al, 2015;Nayak et al, 2014), carbonyl chlorides (Sun et al, 2001;Kudelko et al, 2020), aldehydes (Shivakumara et al, 2019;Wang et al, 2019), etc. We chose here a method based on the transformation of carbonitriles (as shown in the scheme) as the shortest and most convenient way to achieve this purpose (Sakthivel et al, 2016;Abdelhamid et al, 2011). Its efficacy has recently been demonstrated by one of us (Petkevich et al, 2021).…”

Green and practical transition metal-free one-pot conversion of substituted benzoic acids to anilines using tosyl azide

“…Recently, several other C-H functionalisation approaches to access anilines were also reported. 22 During a recent study on the synthesis of biologically active heterocycles 23 we examined Pd-catalyzed ortho-C-H amidation 24 of pyranochromanone acid 6a using p-toluenesulphonyl azide (tosyl azide, TsN 3 ) and K 2 CO 3 in DMF (Scheme 3). We were delighted to find the formation of pyranochromanone aniline t-7a instead of ortho-C-H amidation product 8.…”