Yu, Qian published the artcileSynthesis, cytotoxicity and structure-activity relationship of indolizinoquinolinedione derivatives as DNA topoisomerase IB catalytic inhibitors, Category: alcohols-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2018), 195-207, database is CAplus and MEDLINE.
A series of indolizinoquinolinedione derivatives I [X1 = N; X2 = X3 = X4 = CH; n = 2, 3; R1 = H, F, Cl; R2 = NMe2, pyrrolidinyl, piperidinyl, morpholinyl, 4-methylpiperazinyl] and II [R3 = NMe2, pyrrolidinyl, piperidinyl, morpholinyl] was synthesized. TOP1-mediated relaxation, nicking and unwinding assays revealed that three fluorinated derivatives I [X1 = N; X2 = X3 = X4 = CH; n = 2, 3; R1 = F; R2 = pyrrolidinyl, piperidinyl] and one N,N-trans derivative I [X1 = X2 = X3 = CH; X4 = N; n = 2; R2 = morpholinyl] act as TOP1 catalytic inhibitors with higher TOP1 inhibition (++++) than camptothecin (+++) and without TOP1-mediated unwinding effect. MTT assay against five human cancer cell lines indicated that the highest cytotoxicity was II [R3 = piperidinyl] for CCRF-CEM cells, I [X1 = N; X2 = X3 = X4 = CH; n = 3; R1 = F; R2 = NMe2] for A549 and DU-145 cells, I [X1 = N; X2 = X3 = X4 = CH; n = 2; R1 = F; R2 = pyrrolidinyl] for HCT116 cells, and I [X1 = N; X2 = X3 = X4 = CH; n = 3; R1 = F; R2 = 4-methylpiperazinyl] for Huh7 cells with GI50 values at nanomolar range. The drug-resistant cell assay indicated that compound I [X1 = N; X2 = X3 = X4 = CH; n = 2; R1 = F; R2 = pyrrolidinyl] may mainly act to TOP1 in cells and was less of Pgp substrates. Flow cytometric anal. showed that compounds I [X1 = N; X2 = X3 = X4 = CH; n = 2, 3; R1 = F; R2 = pyrrolidinyl, piperidinyl] could obviously induce apoptosis of HCT116 cells. Moreover, the structure-activity relationship (SAR) of indolizinoquinolinedione derivatives was analyzed.
European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C20H21ClN4O4, Category: alcohols-buliding-blocks.
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