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1.
Biotechnol Appl Biochem ; 63(5): 715-726, 2016 Sep.
Article in English | MEDLINE | ID: mdl-26178774

ABSTRACT

The imminent depletion of fossil fuels and the surging global demand for renewable energy have led to the search for nonconventional energy sources. After a few decades of trial and error, the world is now testing the sources of the third generation of fossil fuels, which contain for most parts microalgae. With more than 80% oil content, being adaptable in growth parameters and highly versatile, microalgae are highly promising sources of biofuels in the present time. The present article makes a sweeping attempt to highlight the various methods employed for cultivation of microalgae, techniques to harvest and extract biomass from huge algal cultures, as well as their downstream production and processing procedures. The advantages, limitations, and challenges faced by each of them have been described to some extent. Major concerns pertaining to biofuels are supposed to be their environmental sustainability and economic viability along with their cost effectiveness. This would require a great deal of empirical data on existing systems and a great deal of optimization to generate a more robust one. We have concluded our article with a SWOT analysis of using algae for biodiesel production in a tabulated form.


Subject(s)
Biofuels/microbiology , Biotechnology/methods , Microalgae/metabolism , Animals , Humans , Microalgae/growth & development
2.
J Med Chem ; 54(8): 3076-80, 2011 Apr 28.
Article in English | MEDLINE | ID: mdl-21434659

ABSTRACT

Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5,6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shuffling of the nitrogen from the N-1 position or by insertion of one or two nitrogen atoms into the indole core of 1. Among these, 7-azaindole core 12 showed potent in vitro anticancer activity and improved oral bioavailability (F = 35%) compared with 1 (F < 10%).


Subject(s)
Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Bridged Bicyclo Compounds/chemical synthesis , Bridged Bicyclo Compounds/pharmacology , Administration, Oral , Antineoplastic Agents/administration & dosage , Biological Availability , Bridged Bicyclo Compounds/administration & dosage , Cell Line, Tumor , Humans
3.
J Med Chem ; 52(4): 1050-62, 2009 Feb 26.
Article in English | MEDLINE | ID: mdl-19140666

ABSTRACT

Aurora kinases have emerged as attractive targets for the design of anticancer drugs. Through structure-based virtual screening, novel pyrazole hit 8a was identified as Aurora kinase A inhibitor (IC(50) = 15.1 microM). X-ray cocrystal structure of 8a in complex with Aurora A protein revealed the C-4 position ethyl carboxylate side chain as a possible modification site for improving the potency. On the basis of this insight, bioisosteric replacement of the ester with amide linkage and changing the ethyl substituent to hydrophobic 3-acetamidophenyl ring led to the identification of 12w with a approximately 450-fold improved Aurora kinase A inhibition potency (IC(50) = 33 nM), compared to 8a. Compound 12w showed selective inhibition of Aurora A kinase over Aurora B/C, which might be due to the presence of a unique H-bond interaction between the 3-acetamido group and the Aurora A nonconserved Thr217 residue, which in Aurora B/C is Glu and found to sterically clash with the 3-acetamido group in modeling studies.


Subject(s)
Antineoplastic Agents/chemistry , Drug Design , Protein Kinase Inhibitors/chemistry , Protein Serine-Threonine Kinases/antagonists & inhibitors , Amides , Antineoplastic Agents/pharmacology , Aurora Kinase A , Aurora Kinase B , Aurora Kinases , Crystallography, X-Ray , Humans , Hydrophobic and Hydrophilic Interactions , Inhibitory Concentration 50 , Molecular Structure , Protein Kinase Inhibitors/pharmacology , Structure-Activity Relationship , Substrate Specificity
4.
ACS Appl Mater Interfaces ; 1(9): 2071-9, 2009 Sep.
Article in English | MEDLINE | ID: mdl-20355835

ABSTRACT

5,7,12,14-Tetrachloro-6,13-diaza-6,13-dihydropentacene (TCDAHP) and 5,7,12,14-tetrachloro-6,13-diazapentacene (TCDAP) were synthesized and assessed as the active channel materials for thin-film transistor applications. Analyses of the crystal structures of these molecules revealed that both exhibited slipped pi-pi stacking of the long and fused aromatic moiety. Although the packing features of the two compounds are basically identical, their highest occupied molecular orbitals, which are relevant to hole transport, are very different. Better mobility was predicted for TCDAHP over TCDAP based on the dimeric structure in the X-ray coordinates. The morphologies of thin films of TCDAHP and TCDAP prepared by thermal evaporation depend critically on the substrate on which the molecules were deposited: from the amorphous state on a SiO(2)/Si surface to the crystalline state on a pentacene buffer layer surface. The performance of thin-film transistors prepared on various substrate surfaces was studied. While no field-effect mobility was observed for these films deposited on SiO(2)/Si, a high mobility of 1.4 cm(2)/(V s) for the TCDAHP film was achieved when deposited on a pentacene buffer layer prepared on a rubbed monolayer of n-nonyltrichlorosilane on a SiO(2)/Si surface. A similar device prepared from TCDAP gave a mobility of 0.13 cm(2)/(V s).

5.
Org Lett ; 8(13): 2867-9, 2006 Jun 22.
Article in English | MEDLINE | ID: mdl-16774277

ABSTRACT

[reaction: see text] o-Iodoaryl aldehydes react with bicyclic alkenes in the presence of NiBr(2)(dppe) and Zn powder in acetonitrile at 80 degrees C undergoing annulation to give polycyclic ketone derivatives. Surprisingly, o-iodoaryl alkyl ketones also react with bicyclic alkenes to form polycyclic ketones with structures the same as those from the corresponding o-iodoaryl aldehydes.

6.
J Org Chem ; 71(2): 655-8, 2006 Jan 20.
Article in English | MEDLINE | ID: mdl-16408976

ABSTRACT

[reaction: see text] An efficient cobalt-catalyzed reductive coupling reaction of alkyl halides with electron-withdrawing alkenes (CH(2)=CR(1)EWG, EWG = electron-withdrawing group) in the presence of water and zinc powder in acetonitrile to give the corresponding Michael-type addition product (RCH(2)CR(1)EWG) was described. The methodology is versatile such that unactivated primary, secondary, and tertiary alkyl bromides and iodides and various conjugated alkenes including acrylates, acrylonitrile, methyl vinyl ketone, and vinyl sulfone all successfully participate in this coupling reaction. For the alkyl halides used in the reaction, the iodides generally gave better yields compared to those of the corresponding bromides. It is a unique method employing CoI(2)dppe, zinc, and alkyl halides, affording conjugate addition products in high yields. Mechanistically, the reaction appears to follow an oxidative addition driven route rather than the previously reported radical route.

7.
Org Lett ; 5(25): 4903-6, 2003 Dec 11.
Article in English | MEDLINE | ID: mdl-14653703

ABSTRACT

In the presence of Ni(dppe)Br(2) and Zn powder in acetonitrile at 80 degrees C, oxa-bicyclic olefins undergo cyclization with o-iodobenzoate and with beta-iodo-(Z)-propenoates to give the benzocoumarin derivatives in moderate to good yields. This methodology offers a simple efficient way for the synthesis of structurally complicate coumarins in one pot. [reaction: see text]

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