21703-08-2Relevant academic research and scientific papers
BIGUANIDE COMPOUNDS AND USE THEREOF
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Paragraph 0524-0527; 0533-0537, (2021/02/16)
The present invention relates to a biguanide compound and uses thereof. More specifically, the present invention relates to: a biguanide derivative exhibiting excellent effects in inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a manufacturing method of the biguanide derivative; and a pharmaceutical composition containing the biguanide derivative as an active component.
Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors
Landi, Giacomo,Linciano, Pasquale,Borsari, Chiara,Bertolacini, Claudia P.,Moraes, Carolina B.,Cordeiro-Da-Silva, Anabela,Gul, Sheraz,Witt, Gesa,Kuzikov, Maria,Costi, Maria Paola,Pozzi, Cecilia,Mangani, Stefano
, p. 1105 - 1114 (2019/05/22)
Cycloguanil is a known dihydrofolate-reductase (DHFR) inhibitor, but there is no evidence of its activity on pteridine reductase (PTR), the main metabolic bypass to DHFR inhibition in trypanosomatid parasites. Here, we provide experimental evidence of cycloguanil as an inhibitor of Trypanosoma brucei PTR1 (TbPTR1). A small library of cycloguanil derivatives was developed, resulting in 1 and 2a having IC50 values of 692 and 186 nM, respectively, toward TbPTR1. Structural analysis revealed that the increased potency of 1 and 2a is due to the combined contributions of hydrophobic interactions, H-bonds, and halogen bonds. Moreover, in vitro cell-growth-inhibition tests indicated that 2a is also effective on T. brucei. The simultaneous inhibition of DHFR and PTR1 activity in T. brucei is a promising new strategy for the treatment of human African trypanosomiasis. For this purpose, 1,6-dihydrotriazines represent new molecular tools to develop potent dual PTR and DHFR inhibitors.
BIGUANIDE COMPOUNDS AND USE THEREOF
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Paragraph 0356; 0357; 0362; 0363, (2015/05/13)
The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for pre
