Gummidi, Lalitha; Kerru, Nagaraju; Awolade, Paul; Raza, Asif; Sharma, Arun K.; Singh, Parvesh published the artcile< Synthesis of indole-tethered [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids as anti-pancreatic cancer agents>, Synthetic Route of 70057-67-9, the main research area is indole tethered thiadiazolo oxadiazolopyrimidinone hydrid preparation antitumor agent; Indole; Molecular hybridization; Pancreatic cancer; Pyrimidinone; [4+2] Cycloaddition reaction.
New indole-tethered [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one (e.g. I) and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (e.g. II) were synthesized using [4+2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with indole-ketenes. All mol. hybrids were structurally characterized by spectroscopic techniques (IR, NMR, and HRMS) and screened for their anti-pancreatic cancer activity in vitro. The [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids showed stronger anti-pancreatic cancer activity than the [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one hybrids against the PANC-1 cell line. II bearing an ortho-chlorophenyl moiety emerged as the most potent anti-pancreatic cancer agent with an IC50 value of 7.7 ± 0.4μM, much superior to the standard drug Gemcitabine (IC50 > 500μM). The discovery of these [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids elicits their potentials as pursuable candidates for pancreatic cancer chemotherapy.
Bioorganic & Medicinal Chemistry Letters published new progress about [4+2] Cycloaddition reaction. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Synthetic Route of 70057-67-9.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics