6. / BRIEF RESUME OF INTENDED WORK:
6.1: NEED FOR THE STUDY:
Angiogenesis is the formation of new blood vessels. Tumors need blood vessels to grow and spread [1].
The process of angiogenesis is controlled by chemical signals in the body. These signals can stimulate both the repair of damaged blood vessels and the formation of new blood vessels.
Angiogenesis inhibitors are designed to prevent the formation of new blood vessels, thereby stopping or slowing the growth or spread of tumors.
The U.S. Food and Drug Administration has approved several angiogenesis inhibitors for the treatment of cancer.
Research on angiogenesis inhibition as a therapeutic strategy against cancer started around 1971, when Folk man postulated that tumor growth is dependent on angiogenesis.
 In the past two decades, inhibitors of angiogenesis have been developed for clinical use. Most notable angiogenesis inhibitors target the vascular endothelial growth factor signaling pathway, such as the monoclonal antibody bevacizumab and two kinase inhibitors sunitinib and sorafenib.
Bevacizumab was the first angiogenesis inhibitor that was clinically approved, initially for treatment of colorectal cancer and recently also for breast cancer and lung cancer.
Angiogenesis inhibitor therapy does not necessarily kill tumors but instead may prevent tumors from growing. Therefore, this type of therapy may need to be administered over a long period.
Angiogenesis inhibitors may have side effects that are different from those of other cancer treatments. In addition, they may only stop or slow the growth of a cancer, not completely eradicate it.
Quinazolineis aheterocyclic compoundmade up of two fused ringssuch asabenzenering and pyrimidinering[2].
Quinazolinone derivatives are known to possess a broad spectrum of biological activities and are used in pharmaceutical industry, in medicine and agriculture.
Quinazolinone derivatives have recently gained a growing interest owing to their reported biological activities. Among these activities, their uses as inflammatory[3] antimicrobial.[4], antitumor[5], and many other pharmacological action, these derivatives are also used in dye industries
The above mentioned biological activities together with the industrial importance of this class of compounds and our interest in this field stimulate us to synthesise several new quinazolinone derivatives and studying the antiangiogeneses activities of some compounds.
6.2: REVIEW OF LITERATURE:
Omar ABDand co-workers have reported the Synthesis of new series of some 2-[(E)-2-furan-2-yl-vinyl]-quinazolin-4(3H)-ones incorporated into pyrazoline, isoxazoline, pyrimidine or pyrimidine-thione ring systems at position-3 of the quinazoline ring. The antimicrobial activity and anti-inflammatory effect of these compounds were carried out.[6].
Adel S et al., have worked extensively on novel derivatives of quinazoline for their antitumor activity against three tumor cell lines among these cell lines the human breast carcinoma cell line in which EGFR is highly expressed. All tested compounds showed potent and selective activity against breast cancer. Virtual screening was carried out through docking the designed compounds into the ATP binding site of epidermal growth factor receptor to predict antitumor activity [7].
Subran et al., have adopted one-pot synthetic methodology to synthesis final compounds. A set of six Schiff bases were synthesized by reacting 2-(4-substituted)phenyl-3-aminoquinazoline-4-3(H)one and 2-Phenyl-3-aminoquinazoline -4-3(H)one with various substituted aromatic aldehydes in glass vials and placed in an oil bath at 800C. Structural elucidation was done by spectroscopic method. The final compounds were screened for their antimicrobial activity[8].
Aly have reported a highly efficient and versatile synthetic approach to the synthesis of annulated quinazoline derivatives also, a variety of pyrazolylquinazolinesand pyrimidinylquinazolines. The new compounds were synthesized with the objective of studying their antimicrobial activity [9].
Rajveer et al., have been synthesized a number of oxoquinazoline derivatives, purified and characterized with the help of their analytical and spectral data (IR,NMR & Mass). The synthesized compounds were screened for their antibacterial Activity and anti-inflammatory activity by standard method [10].
Sarika et al., have been reported an efficient and extremely fast procedure for the synthesis of 7,11-Diphenyl5,6a,7,11,11a,13a-hexahydro-6H-benzo[h]isoxazolo
[3',4',4,5][1,3]thiazolo[2,3-b]quinazolines through four-step procedure starting from 2-arylidenetetralin-1-one under microwave irradiation is reported. A considerable increase in the reaction rate has been observed with better yield. The structures of the synthesized compounds have been characterized on the basis of their elemental analysis and spectral data. Synthesized compounds evaluated for theirantimicrobial activity [11].
Adel et al., were prepared two new series of 6-iodo-2,4-dithio-4(3H)quinazoline and
6-iodo-2-thio-4-oxo-quinazoline and screened for their antimicrobial activity [12].
Dodiya Dk and co-workershave synthesized novel 4-aryl-5,5=dimethyl-7-(2-iperidin-1-yl-ethyl)2-hydroxy-3,4,5,6-tetrahydroquinazolinederivatives and screened for anti tubercular and antimicrobial activities[13].
Literature study revealed that synthesis of quinazoline-2-thiols have been reported by kaur et al., These were synthesized by the condensation of 2-[isothiocyanato(substitutedphenyl)methyl]-3,4-dihydronaphthalene-1(2H)-onewith primary aromatic amines[14].
Ghadamali et al., were synthesizedsome fused quinazolinone derivatives. Based on the biological properties of quinazolinone the activity such as antibacterial, anticancer, and anti-inflammatory activity were carried out . Deoxyvasicinone which was previously synthesized by a multi-step complex reactions was prepared in three steps .The synthesized compounds were evaluated against six strains of bacteria (three Gram-positive and three Gram-negative) and three strains of fungi [15].
Mohammed was carried out the structure activity relationship and biochemical effects of some novel triazoloquinazolines and azinoquinazolines containing sulfacetamide moiety. Some of the newly synthesized compounds showed good anti-inflammatory activities [16].
6.3 MAIN OBJECTIVE OF THE STUDY :
The main aim of present work is an attempt to,
Design and Synthesis of novel quinazoline derivatives .

where R1 = CH3, C2H5
R2 =CH3, C2H5
Characterization of all the synthesized compounds using physical constant, TLC, Elemental analysis and Spectroscopic methods (IR, 1HNMR and Mass spectrum).
Evaluation of the synthesized compounds for their anti-angiogenesis activity.
7. / MATERIALS & METHODS
7.1 SOURCE OF THE DATA:
The Preliminary data required for the experimental study was obtained from
Library, Govt. College of Pharmacy Bengaluru.
Library and Information Centre, Rajiv Gandhi University of Health Science, Bengaluru.
 direct.
JRD TATA memorial Library IISc. Bengaluru.
Journals and e-journals.
7.2 METHODS OF COLLECTION OF DATA:
  1. The experimental data will be obtained by experimenting in the laboratories of Department of Pharmaceutical Chemistry Govt. College of Pharmacy Bengaluru.
7.3 DOES THE STUDY REQUIRE ANY INVESTIGATIONS OR INTERVENTIONS TO BE CONDUCTED ON ANIMALS? IF SO, PLEASE DESCRIBE IN BRIEF.
NOT APPLICABLE
7.4 HAS ETHICAL CLEARANCE BEEN OBTAINED FROM YOUR INSTITUTE IN CASE 7.3?
NOT APPLICABLE
8. / LIST OF REFERENCES:
1.Kristy JGandHenk MW. Anti-angiogenic tyrosine kinase inhibitors for the treatment of tumor . Springer Angiogenesis.2010; 13(1):1–14.
2.Nahed F and Abdel G.Synthesis and Biological Evaluation of Some Nitrogen Containing Heterocycles.Nat Sci.2011;9(7):190-201.
3.Alafeefy AM,Kadi AA,Al-Deeb OA,El-Tahir KE and Al-Jaber NA. Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives.Eur J Med Chem.2010;45(11):4947-52.
4.Hemdan, Magdy M,Fahmy, Amin F,El-Sayed and Amira A.s
5.Synthesis and antimicrobial study of 1, 2, 4-triazole, quinazoline and benzothiazole derivatives from 1-naphthoylisothiocyanate.J Chem Res.2010; 34(4):219-21.
6.Vedula MS, Prasanna A, Adi KV,Renuka B, Laxman CV and Sunil Kumar G et al., Novel Indolo[2,1-b]quinazoline Analogues as Cytostatic Agents: Synthesis, Biological Evaluation and Structure–Activity Relationship. Bioorg Med Chem Lett.2002;(12):2303–307.
7.Fathalla M, Emad MM, Kassem NM, Ibrahem and Mohsen MK. Synthesis of Some New Quinazolin-4-One Derivatives and Evaluation of their Antimicrobial and Antiinflammatory effects. Acta Pol Pharm Drug Res. 2008;65(1):11-20.
8.Adel SA, Mohamed AO, Alaa AMA, Naglaa IA, Magda AA, Abdulaziz MA, Sayed-MA and Sami GA et al., Design, Synthesis and Biological Evaluation of Novel Quinazoline Derivatives as Potential Antitumor Agents Molecular Docking Study. Eur J Med Chem.2010;45:4188-98.
9.Subarna G, Panigrahi MK, Pratiksha S and Shukla PK. One-Pot Synthesis of Novel Quinazoline Derivatives and their Antimicrobial Activity. Int J Pharm Pharm Sci.2012;4(4):434-40.
10.Aly AA. Synthesis and Antimicrobial Activity of Some Annelated Quinazoline Derivatives. J Chin Chem Soc. 2007;54: 437-46.
11.Rajveer CH, Stephen R, Kumaraswamy D, Sudharshini S, Swarnalatha CH, and Preetha SP. Synthesis and Biological Evaluation of Some Novel Oxo-Quinazoline Derivatives for their AntiBacterial Activity.Res J Pharm Bio Chem Sci. 2010;1(2): 366-71.
12.Sarika M, Neelam S, Madhuri V, Jitendra V, Pinki BP and Suresh CA. Synthesis and Characterization of Some Quinazoline Derivatives as Potential Antimicrobial Agents under Microwave Irradiation. Bull Kor Chem Soc.2007; 28(12):2338-342.
13.Adel SE, Adnan AK, Ahmed M, Alafeefy and Abdel SG. Synthesis of Some New Quinazoline Analogs and their Antimicrobial Activity.Saudi Pharm J 2001; 9:72-84.
14.Dodiya DK, Vaghasia SJ, Trivedi AR, Ram HK and Shah VH. Synthesis, characterization and Biological Screening of Some Novel Tetrahydroquinazoline Derivatives. Ind J chem. 2010;49(B):802-06.
15.Kaur R, Bansal M and Kaur B. Synthesis of Some New Quinazoline Derivatives and Theoretical Studies of their Geometries. Chem Sci J.2011;18:1-9.
16.Ghadamali K, Elham J, Gholamhossein H, Daryoush A, Marzieh RKand Farshid H.Synthesis of Some New Quinazolinone Derivatives and Evaluation of Their Antimicrobial Activities. Iranian J Pharm Res.2012;11(3):789-97.
17.Mohammed AH. Structure Anti-Inflammatory Activity Relationship and Biochemical Valuation of Some Novel Triazoloquinazoline and Triazinoquinazoline Derivatives Containing Sulfacetamide Moiety.Int J Appl Biol Pharm Technol.2010;1(3):1054-66.
9. / SIGNATURE OF THE CANDIDATE: / (DEVARAJA.M)
10. / REMARKS OF THE GUIDE:
11. / NAME AND DESIGNATION OF:
11.1 GUIDE: / Mr. ZARANAPPA
ASST PROFESSOR,
DEPT. OF PHARMACEUTICAL CHEMISTRY,
GOVERNMENT COLLEGE OF PHARMACY,
BENGALUR/U – 560027.
11.2 SIGNATURE:
11.3 CO- GUIDE
11.4 SIGNATURE:
11.5 HEAD OF THE DEPARTMENT: / PROF. M.S. NIRANJAN
HEAD OF THE DEPARTMENT,
DEPT. OF PHARMACEUTICAL CHEMISTRY,
GOVERNMENT COLLEGE OF PHARMACY,
BENGALURU – 560 027.
11.4 SIGNATURE:
12 / 12.1 REMARKS OF THE CHAIRMAN AND PRINCIPAL:
12.2 SIGNATURE: / DR.S. SHASHIDHARA
PRINCIPAL
GOVERNMENT COLLEGE OF
PHARMACY
BANGALURE-560027.