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Asgari, Davoud,Aghanejad, Ayuob,Mojarrad, Javid Shahbazi Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized.
Biodiversity status of Tulipa (Liliaceae) in Iran inferred from molecular characterization
Davoud Asgari,Alireza Babaei,Mohammad Reza Naghavi,Mahmoud Kiani 한국원예학회 2020 Horticulture, Environment, and Biotechnology Vol.61 No.3
Here, we used data generated from amplifi ed fragment length polymorphism (AFLP) analysis to address the biodiversitystatus and taxonomic relationships among 47 wild accessions representing 9 species of the genus Tulipa in Iran. A high levelof genetic diversity within the genus was observed; the most distant taxa were T. humilis and T. schrenkii , while the highestdegree of similarity was found between T. montana and T. bifl ora . Twelve AFLP primer sets amplifi ed 342 fragments, ofwhich 304 were polymorphic (88.1%). The average number of polymorphic bands per AFLP primer pair was 28.5. A hierarchicalcluster analysis was carried out on the genetic profi le of the taxa, and the results mostly reconfi rmed the recognizedtaxonomy of the genus. However, we found evidence for recognition of a new subgenus for T. biebersteiniana .
Davoud Asgari,Ayuob Aghanejad,Javid Shahbazi Mojarrad 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized.
Synthesis, Characterization and in vitro Anti-Tumoral Evaluation of Erlotinib-PCEC Nanoparticles
Barghi, Leila,Asgari, Davoud,Barar, Jaleh,Nakhlband, Aylar,Valizadeh, Hadi Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.23
Background: Development of a nanosized polymeric delivery system for erlotinib was the main objective of this research. Materials and Methods: Poly caprolactone-polyethylene glycol-polycaprolactone (PCEC) copolymers with different compositions were synthesized via ring opening polymerization. Formation of triblock copolymers was confirmed by HNMR as well as FT-IR. Erlotinib loaded nanoparticles were prepared by means of synthesized copolymers with solvent displacement method. Results: Physicochemical properties of obtained polymeric nanoparticles were dependent on composition of used copolymers. Size of particles was decreased with decreasing the PCL/PEG molar ratio in used copolymers. Encapsulation efficiency of prepared formulations was declined by decreasing their particle size. Drug release behavior from the prepared nanoparticles exhibited a sustained pattern without a burst release. From the release profiles, it can be found that erlotinib release rate from polymeric nanoparticles is decreased by increase of CL/PEG molar ratio of prepared block copolymers. Based on MTT assay results, cell growth inhibition of erlotinib has a dose and time dependent pattern. After 72 hours of exposure, the 50% inhibitory concentration (IC50) of erlotinib hydrochloride was appeared to be $14.8{\mu}M$. Conclusions: From the obtained results, it can be concluded that the prepared PCEC nanoparticles in this study might have the potential to be considered as delivery system for erlotinib.
Covalent Immobilization of Trypsin on a Novel Aldehyde-Terminated PAMAM Dendrimer
Aliasghar Hamidi,Mohammad R. Rashidi,Davoud Asgari,Ayuob Aghanejad,Soodabeh Davaran 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.7
Dendrimers are a novel class of nonlinear polymers and due to their extensive applications in different fields, called versatile polymers. Polyamidoamine (PAMAM) dendrimers are one of the most important dendrimers that have many applications in nanobiotechnology and industry. Generally aldehyde terminated dendrimers are prepared by activation of amine terminated dendrimers by glutaraldehyde which has two problems, toxicity and possibility of crosslink formation. In this study, novel aldehyde-terminated PAMAM dendrimer was prepared and used for covalent immobilization of trypsin by the aim of finding a special reagent which can prevent crosslinking and deactivation of the enzyme. For this purpose aminoacetaldehydedimethylacetal (AADA) was used as spacer group between aldehyde-terminated PAMAM and trypsin.The findings of this study showed that immobilization of trypsin not only resulted higher optimal temperature, but also increased the thermal stability of the immobilized enzyme in comparison to the free enzyme.
Covalent Immobilization of Trypsin on a Novel Aldehyde-Terminated PAMAM Dendrimer
Hamidi, Aliasghar,Rashidi, Mohammad R.,Asgari, Davoud,Aghanejad, Ayuob,Davaran, Soodabeh Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.7
Dendrimers are a novel class of nonlinear polymers and due to their extensive applications in different fields, called versatile polymers. Polyamidoamine (PAMAM) dendrimers are one of the most important dendrimers that have many applications in nanobiotechnology and industry. Generally aldehyde terminated dendrimers are prepared by activation of amine terminated dendrimers by glutaraldehyde which has two problems, toxicity and possibility of crosslink formation. In this study, novel aldehyde-terminated PAMAM dendrimer was prepared and used for covalent immobilization of trypsin by the aim of finding a special reagent which can prevent crosslinking and deactivation of the enzyme. For this purpose aminoacetaldehydedimethylacetal (AADA) was used as spacer group between aldehyde-terminated PAMAM and trypsin.The findings of this study showed that immobilization of trypsin not only resulted higher optimal temperature, but also increased the thermal stability of the immobilized enzyme in comparison to the free enzyme.