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( Fatemeh Davami ),( Soroush Sardari ),( Keivan Majidzadeh A ),( Mahdi Hemayatkar ),( Farzaneh Barkhordari ),( Somayeh Enayati ),( Ahmad Adeli ),( Fereidoun Mahboudi ) 생화학분자생물학회(구 한국생화학분자생물학회) 2011 BMB Reports Vol.44 No.1
Resistance to PAI-1 is a factor which confers clinical benefits in thrombolytic therapy. The only US FDA approved PAI-1 resistant drug is Tenecteplase(R). Deletion variants of t-PA have the advantage of fewer disulfide bonds in addition to higher plasma half lives. A new variant was developed by deletion of the first three domains in t-PA in addition to substitution of KHRR 128-131 amino acids with AAAA in truncated t-PA. The specific activity of this new variant, 570 IU/μg, was found to be similar to those found in full length t-PA (Alteplase(R)), 580 IU/μg. A 65% and 85% residual activity after inhibition by rPAI-1 was observed for full length and truncated-mutant form, respectively. This new variant as the first PAI-1 resistant truncated t-PA may offer more advantages in clinical conditions in which high PAI-1 levels makes the thrombolytic system prone to re-occlusion. [BMB reports 2011; 44(1): 34-39]
Synthesis, antimycobacterial and anticancer activity of novel indole-based thiosemicarbazones
Vida Mashayekhi,Kamaleddin Haj Mohammad Ebrahim Tehrani,Parisa Azerang,Soroush Sardari,Farzad Kobarfard 대한약학회 2021 Archives of Pharmacal Research Vol.44 No.8
Based on the structural elements of bioactiveindole-based compounds, a series of novel 1-substitutedindole-3-carboxaldehyde thiosemicarbazones were synthesizedas potential antimycobacterial and anticancer agents. The derivatives were prepared via a two-step methodologyincluding N-alkylation(benzylation) of indole-3-carboxaldehydeand conversion of the intermediate aldehydes tocorresponding thiosemicarbazones. The derivatives wereevaluated for their antimycobacterial activity and compounds3d (R = propyl) and 3q (R = 4-nitrobenzyl) wereamong the most potent and selective derivatives with IC50values of 0.9 and 1.9 lg/mL respectively. The anticanceractivity of the derivatives was also assessed against a panelof tumor cell lines. Compounds 3t, 3u, 3v and 3w efficiently inhibited the majority of the cancer cell lineswith considerable selectivity.