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Synthesis and Acetylcholinesterase Inhibitory Activity of Novel Trilaciclib Analogs
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AbstractTrilaciclib is a CDK4/6 inhibitor, used to treat the bone marrow damage in chemotherapy patients. A series of thirteen novel structural trilaciclib analogs was obtained to evaluate their activity against acetylcholinesterase. An effective method for the synthesis of 4,7‐substituted 8,9‐dihydropyrazino[1’,2’:1,5]pyrrolo[2,3‐d]pyrimidine derivatives from a new methyl 4‐chloro‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxylate was developed. Most of the synthesized pyrazino[1’,2’:1,5]pyrrolo[2,3‐d]pyrimidine derivatives inhibited acetylcholinesterase in the micromolar range. The obtained data can be used for designing more potent acetylcholinesterase inhibitors with the pyrazino[1’,2’:1,5]pyrrolo[2,3‐d]pyrimidine scaffold.
Title: Synthesis and Acetylcholinesterase Inhibitory Activity of Novel Trilaciclib Analogs
Description:
AbstractTrilaciclib is a CDK4/6 inhibitor, used to treat the bone marrow damage in chemotherapy patients.
A series of thirteen novel structural trilaciclib analogs was obtained to evaluate their activity against acetylcholinesterase.
An effective method for the synthesis of 4,7‐substituted 8,9‐dihydropyrazino[1’,2’:1,5]pyrrolo[2,3‐d]pyrimidine derivatives from a new methyl 4‐chloro‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxylate was developed.
Most of the synthesized pyrazino[1’,2’:1,5]pyrrolo[2,3‐d]pyrimidine derivatives inhibited acetylcholinesterase in the micromolar range.
The obtained data can be used for designing more potent acetylcholinesterase inhibitors with the pyrazino[1’,2’:1,5]pyrrolo[2,3‐d]pyrimidine scaffold.
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